SMI-4a

SKU: orb1304581

Description

(Z)-SMI-4a, also known as TCS PIM-1 4a, is a potent and selective ATP-competitive inhibitor targeting Pim-1 kinase, exhibiting an IC50 value of 21 nM. This compound is a valuable research tool for investigating Pim-1's role in oncology and hematology, with utility in both cellular and biochemical studies.

Research Area

Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 438190-29-5
• MW: 273.23
• Purity: >98%
• Formula: C₁₁H₆F₃NO₂S
• SMILES: FC(F)(F)C1=CC=CC(\C=C2\SC(=O)NC2=O)=C1
• Target: Kinase
• Solubility: Soluble in DMSO (up to 100 mg/ml) or in Ethanol (up to 40 mg/ml with warming).

Bioactivity

• Target IC50:
  PIM2:100 μM|Pim1:21 nM
• In Vivo:
  5 μM SMI-4a inhibited the growth of pancreatic cancer and leukemia cells.SMI-4a decreased the phosphorylation of Pim targets in prostate and hematopoietic cells.SMI-4a induced cell cycle arrest and reversed the anti-apoptotic activity of Pim-1.SMI-4a is an ATP-competitive inhibitor of Pim1, with an IC50 of 17 nM.SMI-4a demonstrated high selectivity for a panel of kinases by Pim1. SMI-4a inhibited the in vitro phosphorylation of Pim-1 by a known substrate, the translation blocker 4E-BP1.SMI-4a increased the amount of p27Kip1 in the nucleus.SMI-4a treatment induced the up-regulation of the MAPK pathway.SMI-4a inhibited the mTOR pathway by treatment of pre-T-LBL.SMI-4a inhibited the mTOR pathway by treatment of pre-T-LBL.
• In Vitro:
  5 μM SMI-4a inhibited the growth of pancreatic cancer and leukemia cells.SMI-4a decreased the phosphorylation of Pim targets in prostate and hematopoietic cells.SMI-4a induced cell cycle arrest and reversed the anti-apoptotic activity of Pim-1.SMI-4a is an ATP-competitive inhibitor of Pim1, with an IC50 of 17 nM.SMI-4a demonstrated high selectivity for a panel of kinases by Pim1. SMI-4a inhibited the in vitro phosphorylation of Pim-1 by a known substrate, the translation blocker 4E-BP1.SMI-4a increased the amount of p27Kip1 in the nucleus.SMI-4a treatment induced the up-regulation of the MAPK pathway.SMI-4a inhibited the mTOR pathway by treatment of pre-T-LBL.SMI-4a inhibited the mTOR pathway by treatment of pre-T-LBL.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cell-permeable, 4E-BP1, (Z)SMI4a, (Z) SMI 4a, Pim-2, Pim, Pim1, Pim-1, SMI-4a, TCS PIM-1 4a

Compound Identifiers

PubChem CID

1361332